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公开(公告)号：US10292987B2
公开(公告)日：2019-05-21
申请号：US15459141
申请日：2017-03-15
Inventor： Jae U. Jeong , Deepak Bandyopadhyay , Patrick M. Eidam , Philip Anthony Harris , Jianxing Kang , Bryan Wayne King , Ami Lakdawala Shah , Lara Kathryn Leister , Attiq Rahman , Joshi M. Ramanjulu , Clark A. Sehon , Robert Singhaus, Jr. , Daohua Zhang
IPC: A61K31/553 , C07D267/14 , C07D403/12 , C07D413/14 , C07D403/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/04 , C07D498/04 , C07D281/10 , A61K31/55 , C07D223/08
Abstract: Disclosed are compounds having the formula: wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A. L, and B are as defined herein, and methods of making and using the same.
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公开(公告)号：US10975056B2
公开(公告)日：2021-04-13
申请号：US16309121
申请日：2017-06-13
Applicant: GlaxoSmithKline Intellectual Property Development Limited , Cancer Research Technology Ltd.
Inventor： Nicholas David Adams , Andrew B. Benowitz , María Lourdes Rueda Benede , Karen Anderson Evans , David T Fosbenner , Bryan Wayne King , Mei Li , Juan Ignacio Luengo , William Henry Miller , Alexander Joseph Reif , Stuart Paul Romeril , Stanley J. Schmidt , Roger J. Butlin , Kristin M. Goldberg , Allan M. Jordan , Christopher S. Kershaw , Ali Raoof , Bohdan Waszkowycz
IPC: C07D401/12 , C07D401/04 , C07D213/73 , C07D213/74 , C07D413/14 , C07D417/12 , A61P37/00 , A61P35/00 , C07D401/14
Abstract: The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): wherein Yar, X1ar, X2ar, R1ar, R2ar, R3ar, R4ar and R5ar are as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compounds of the invention are selective inhibitors of DNMT1 and can be useful in the treatment of cancer, pre-cancerous syndromes, beta hemoglobinopathy disorders, sickle cell disease, sickle cell anemia, and beta thalassemia, and diseases associated with DNMT1 inhibition. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
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公开(公告)号：US09556152B2
公开(公告)日：2017-01-31
申请号：US14763183
申请日：2014-02-14
Inventor： Philip Anthony Harris , Bryan Wayne King
IPC: A61K31/553 , C07D267/14 , C07D403/12 , C07D413/14 , C07D403/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/04 , C07D498/04 , C07D281/10
CPC classification number: A61K31/553 , A61K31/55 , C07D223/08 , C07D267/14 , C07D281/10 , C07D403/12 , C07D403/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/04 , C07D498/04
Abstract: Disclosed are compounds having the formula: wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A, L, and B are as defined herein, and methods of making and using the same.
Abstract translation: 公开了具有下式的化合物：其中X，Y，Z1，Z2，Z3，Z4，R5，RA，m，A，L和B如本文所定义，以及制备和使用它们的方法。
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公开(公告)号：US20230101987A1
公开(公告)日：2023-03-30
申请号：US17966504
申请日：2022-10-14
Inventor： Andrew B. BENOWITZ , David T. Fosbenner , Bryan Wayne King , Stuart Paul Romeril
IPC: A61K31/675 , C07F9/58 , C07D213/85 , A61P35/02 , A61K31/44
Abstract: The invention relates to substituted pyridine derivatives that are inhibitors of the activity of DNA methyltransferase 1 (DNMT1). The invention also relates to pharmaceutical compositions comprising such compounds and methods of using such compounds in the treatment of cancer, pre-cancerous syndromes, beta haemoglobinopathy disorders, and other diseases associated with inappropriate DNMT1 activity.
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公开(公告)号：US20190201413A1
公开(公告)日：2019-07-04
申请号：US16299254
申请日：2019-03-12
Inventor： Jae U. JEONG , Deepak Bandyopadhyay , Patrick M. Eidam , Philip Anthony Harris , Jianxing Kang , Bryan Wayne King , Ami Lakdawala Shah , Lara Kathryn Leister , Attiq Rahman , Joshi M. Ramanjulu , Clark A. Sehon , Robert Singhaus, JR. , Daohua Zhang
IPC: A61K31/553 , A61K31/55 , C07D403/12 , C07D223/08 , C07D281/10 , C07D498/04 , C07D413/14 , C07D487/04 , C07D417/12 , C07D413/12 , C07D409/12 , C07D403/14 , C07D267/14
CPC classification number: A61K31/553 , A61K31/55 , C07D223/08 , C07D267/14 , C07D281/10 , C07D403/12 , C07D403/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/04 , C07D498/04
Abstract: Disclosed are compounds having the formula: wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A. L, and B are as defined herein, and methods of making and using the same.
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Patent Agency Ranking
![TRIAZOLE-SUBSTITUTED IMIDAZO[1,2-A]PYRIMIDINES AS CGAS INHIBITORS](/abs-image/US/2025/03/20/US20250092053A1/abs.jpg.150x150.jpg)
公开(公告)号：US20250092053A1
公开(公告)日：2025-03-20
申请号：US18966276
申请日：2024-12-03
Inventor： Adam K. CHARNLEY , Janos Botyanszki , Xiaoyang Dong , Philip Gareth Humphreys , Bryan Wayne King , Kimberly Katherine Marcus , Joseph Pero , Alexander Joseph Reif , Daohua Zhang , Attiq Rahman , Kenneth Allen Newlander , Kenneth Wiggall , Joshi Ramanjulu
IPC: C07D487/04 , C07D403/14 , C07D471/04 , C07D471/14 , C07F9/6561
Abstract: The present invention relates to compounds of Formula (I), compositions containing them, and to their use in the treatment of various disorders, in particular autoimmune, autoinflammatory or immune-mediated conditions, such as systemic lupus erythematosus (SLE), cutaneous lupus erythematosus (CLE) and lupus nephritis.
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公开(公告)号：US11771711B2
公开(公告)日：2023-10-03
申请号：US17966504
申请日：2022-10-14
Inventor： Andrew B. Benowitz , David T. Fosbenner , Bryan Wayne King , Stuart Paul Romeril
IPC: A61K31/675 , A61P35/02 , A61K31/44 , C07D213/85 , C07F9/58
CPC classification number: A61K31/675 , A61K31/44 , A61P35/02 , C07D213/85 , C07F9/58 , C07B2200/13
Abstract: The invention relates to substituted pyridine derivatives that are inhibitors of the activity of DNA methyltransferase 1 (DNMT1). The invention also relates to pharmaceutical compositions comprising such compounds and methods of using such compounds in the treatment of cancer, pre-cancerous syndromes, beta haemoglobinopathy disorders, and other diseases associated with inappropriate DNMT1 activity.
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公开(公告)号：US20190262356A1
公开(公告)日：2019-08-29
申请号：US16408718
申请日：2019-05-10
Inventor： Jae U. JEONG , Deepak Bandyopadhyay , Patrick M. Eidam , Philip Anthony Harris , Jianxing Kang , Bryan Wayne King , Ami Lakdawala Shah , Lara Kathryn Leister , Attiq Rahman , Joshi M. Ramanjulu , Clark A. Sehon , Robert Singhaus, JR. , Daohua Zhang
IPC: A61K31/553 , C07D413/14 , C07D403/14 , C07D409/12 , C07D413/12 , C07D417/12 , A61K31/55 , C07D267/14 , C07D498/04 , C07D281/10 , C07D223/08 , C07D403/12 , C07D487/04
Abstract: Disclosed are compounds having the formula: wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A. L, and B are as defined herein, and methods of making and using the same.
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公开(公告)号：US12285436B2
公开(公告)日：2025-04-29
申请号：US18358998
申请日：2023-07-26
Inventor： Andrew B. Benowitz , David T. Fosbenner , Bryan Wayne King , Stuart Paul Romeril , Megan Ketchum , Todd Koretke , Elizabeth Ann Moroz , Grace Price
IPC: A61K31/675 , A61K31/44 , A61P35/02 , C07D213/85 , C07F9/58
Abstract: The invention relates to substituted pyridine derivatives that are inhibitors of the activity of DNA methyltransferase 1 (DNMT1). The invention also relates to pharmaceutical compositions comprising such compounds and methods of using such compounds in the treatment of cancer, pre-cancerous syndromes, beta haemoglobinopathy disorders, and other diseases associated with inappropriate DNMT1 activity.
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![Triazole-substituted imidazo[1,2-a]pyrimidines as cGAS inhibitors](/abs-image/US/2025/03/11/US12247033B2/abs.jpg.150x150.jpg)
公开(公告)号：US12247033B2
公开(公告)日：2025-03-11
申请号：US18586620
申请日：2024-02-26
Inventor： Adam K. Charnley , Janos Botyanszki , Xiaoyang Dong , Philip Gareth Humphreys , Bryan Wayne King , Kimberly Katherine Marcus , Joseph Pero , Alexander Joseph Reif , Daohua Zhang , Attiq Rahman , Kenneth Allen Newlander , Kenneth Wiggall , Joshi Ramanjulu
IPC: C07D487/04 , C07D403/14 , C07D471/04 , C07D471/14 , C07F9/6561
Abstract: The present invention relates to compounds of Formula (I), compositions containing them, and to their use in the treatment of various disorders, in particular autoimmune, autoinflammatory or immune-mediated conditions, such as systemic lupus erythematosus (SLE), cutaneous lupus erythematosus (CLE) and lupus nephritis.
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